ARIPIPRAZOLE PRODRUG COMPOSITIONS Russian patent published in 2024 - IPC A61K31/496 A61K47/14 A61K9/10 A61K9/14 A61P25/18 A61P25/22 A61P25/24 B82Y5/00 

FIELD: medicine; pharmaceutics.

SUBSTANCE: invention refers to pharmaceutics, namely to a method for preparing a prodrug composition of aripiprazole. Method of producing a composition containing: a) a collection of aripiprazole prodrug particles having a volume size (Dv50) of 50–700 nm, b) at least one surface stabilizer containing an adsorbed component which is adsorbed on the surface of the aripiprazole prodrug particles, and a free component of the surface stabilizer which is capable of solubilising the aripiprazole prodrug, where the weight ratio of the aripiprazole prodrug to the surface stabilizer is from 10:1 to 26:1, and where the aripiprazole prodrug has the formula

where n denotes 0 or an integer less than 20; where at least one surface stabilizer is selected from a group consisting of caboxymethyl cellulose and a polyoxyethylene sorbitan fatty acid ester, and where said method includes the following steps: (a) calculating the amount of at least one stabilizer to be added to the composition to ensure that both the adsorbed component and the free surface stabilizer component are present in the composition, at that, for the calculation, methods of approximating the amount of the free component of the surface stabilizer are used; (b) obtaining a set of particles of aripiprazole prodrug with volume size (Dv50) less than 50–700 nm; and (c) mixing the calculated amount of the surface stabilizer with the plurality of aripiprazole prodrug particles so that the adsorbed surface stabilizer component is adsorbed onto the surface of the aripiprazole prodrug particles.

EFFECT: invention described above enables to obtain a prodrug composition of aripiprazole with a surface stabilizer with a substantially improved pharmacokinetic profile.

17 cl, 26 dwg, 18 tbl, 12 ex